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Objective:To establish an HPLC gradient elution method for the determination of isoalantolactone,alantolactone,xan-thotoxol,oxypeucedanin,imperatorin and osthole in Kangfu ointment simultaneously. Methods:Isoalantolactone,alantolactone,xan-thotoxol,oxypeucedanin,imperatorin and osthole were determined by HPLC with a chromatographic column of Agilent TC-C18(250 mm ×4.6 mm,5 μm),the mobile phase was methanol-0.1% formic acid solution with gradient elution at a flow rate of 0.9 ml·min-1. The detection wavelengths were 220 nm and 300 nm. The column temperature was 35℃. Results: The linear range of isoalantolac-tone,alantolactone,xanthotoxol,oxypeucedanin,imperatorin and osthole was 6.16-123.20 μg·ml-1,3.78-75.60 μg·ml-1,1.87-37.40 μg·ml-1,4.06-81.20 μg·ml-1,9.27-185.40 μg·ml-1and 13.89-277.80 μg·ml-1,respectively. The correlation coef-ficient was 0.999 4,0.999 8,0.999 6,0.999 5,0.999 9 and 0.999 7, respectively. The average recovery was 98.04% (RSD=1.06%),97.10%(RSD = 1.53%), 96.73% (RSD = 0.90%), 98.92% (RSD = 1.36%), 99.12% (RSD = 0.83%) and 100.27%(RSD=0.58%),respectively. Conclusion:The method is simple and accurate,which can be used to improve the quality standard for Kangfu ointment.
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Objective: To study the absorption and transportation characteristic of xanthotoxol (1), xanthotoxin (2), imperatorin (3), isoimperatorin (4), cnidilin (5), and isopimpinellin (6), which were classified as the linear type furocoumarins, in a model of Caco-2 cell monolayers in human intestinal epithelium. Methods: Caco-2 (the human colon adenocarcinoma cell lines) cell monolayer was used as an intestinal epithelial cell model. The permeability of the six coumarins from apical side (AP side) to basolateral side (BL side) or from BL side to AP side was evaluated. The concentration of the six coumarins was measured by HPLC coupled with UV detector. Transportation parameters and permeability coefficients (Papp) were then calculated, and P app values were compared with the reported values for model compounds, Propranolol and Atenolol. Based on the absorption and transportation characteristic of coumarins 1-6, and psoralen (7), bergaptol (8), bergaptol-O-β-D-glucopyranoside (9), bergapten (10), nodakenin (11), nodakenetin (12), decuroside V (13), umbelliferone (14), osthole (15), angelol-A (16), and angelol-B (17) in a model of Caco-2 cell monolayer, the relationship of absorption and transportation with diversed chemical structures and lipophilicity was reviewed. Results: In the Caco-2 cell monolayer model, the Papp magnitudes of the linear furocoumarins 1-6 were 10-5 cm/s in the bi-directional transport, which was identical with Propranolol. And the permeability of Caco-2 cell monolayer is mainly via passive absorption. Conclusion: The above-mentioned linear furocoumarins 1-6 are well-absorbed compounds. The results show that a significant Sigmoid dependence of permeability on 1g Papp AP→BL and 1g D at pH 7.35 of all 1-17 furocoumarins can be absorbed across intestinal epithelial cells by passive diffusion mechanism.
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AIM: To study the effects of xanthotoxol (XT) on physiological characteristics and its mechanism in isolated guinea pig atria. METHODS: It was determined by the contractile amplitude,excitability and the spontaneous beats in the right atria,respectively. RESULTS: In the experiment of contractile amplitude,after 15 min of administration of XT 20, 40 and 80 ?mol?L -1 ,the contractile force of left atria was 0.85 , 0.68 ,and 0.48 g,respectively (P
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Aim To investigate the inhibitory effects of xanthotoxol(XT) on neutrophil infiltration and brain edema induced by focal cerebral ischemia-reperfusion injury in rats.Methods Focal cerebral ischemia-reperfusion model in rat was induced by transient occlusion of the middle cerebral artery for 2 hours and followed by 24 hours of reperfusion.XT(2.5,5 and 10 mg?kg-1,ip)was administered at 1 hour and 12 hours after the onset of ischemia,respectively.After 24 hours of reperfusion,the influence of XT on neurological deficit score,brain edema and infarct size were evaluated;the activity of Na+,K+-ATPase,Ca2+-ATPase and myeloperoxidasse(MPO) in the ischemic hemisphere cortex of the middle cerebral artery area was assayed by spectrophotometry;the expression of intercellular adhesion molecule-1(ICAM-1) and E-selectin was measured with immunohistochemistry.Results XT significantly reduced the neurological deficit score,brain edema and infarct size,enhanced activity of Na+,K+-ATPase and Ca2+-ATPas,suppressed the injury-induced upregulation of MPO activity and cell adhesion molecules(ICAM-1 and E-selectin) expression in the brain tissue.Conclusion XT attenuates brain damage following focal cerebral ischemia-reperfusion in rats and its mechanism may partly be due to the inhibition of inflammation and brain edema induced by ischemia-reperfusion.